Bioorganic & Medicinal Chemistry 2009-04-15

Botulinum neurotoxin serotype A inhibitors: small-molecule mercaptoacetamide analogs.

Scott T Moe, Andrew B Thompson, Genessa M Smith, Ross A Fredenburg, Ross L Stein, Alan R Jacobson

文献索引：Bioorg. Med. Chem. 17(8) , 3072-9, (2009)

全文：HTML全文

摘要

Botulinum neurotoxin elicits its paralytic activity through a zinc-dependant metalloprotease that cleaves proteins involved in neurotransmitter release. Currently, no drugs are available to reverse the effects of botulinum intoxication. Herein we report the design of a novel series of mercaptoacetamide small-molecule inhibitors active against botulinum neurotoxin serotype A. These analogs show low micromolar inhibitory activity against the isolated enzyme. Structure-activity relationship studies for a series of mercaptoacetamide analogs of 5-amino-3-phenylpyrazole reveal components essential for potent inhibitory activity.

相关化合物

  • 3-氨基-5-苯基吡唑

相关文献：

Anthranilamide-pyrazolo[1,5-a]pyrimidine conjugates as p53 activators in cervical cancer cells.

2012-08-01

[ChemMedChem 7(8) , 1453-64, (2012)]

An efficient one-step synthesis of heterobiaryl pyrazolo[3,4-b]pyridines via indole ring opening.

2009-11-19

[Org. Lett. 11(22) , 5214-7, (2009)]

The conversion of isothiazoles into pyrazoles using hydrazine. Ioannidou HA and Koutentis PA

[Tetrahedron 65(34) , 7023-7037, (2009)]

Crystal structure of chlorido-tris (3-amino-5-phenyl-1H pyrazole-N2) zinc (II) chloride, [ZnCl (C9H9N3)3] Cl. Jacimovic ZK, et al

[Zeitsch. für Kristall. 226(3) , 397-399, (2011)]

Convenient synthesis of some new pyrazolo [5, 1-c] triazines, isoxazolo [3, 4-d] pyrimidine and pyridine derivatives containing benzofuran moiety. Abdelhamid AO, et al

[Eur. J. Chem. 3(2) , 129-137, (2012)]

更多文献...